| Identification | Back Directory | [Name]
N-Benzyl-2-[6-(2-chloroacetylamino)-benzothiazol-2-ylsulfanyl]-acetamide | [CAS]
1255099-06-9 | [Synonyms]
SKLB163
SKLB-163
SKLB 163
N-Benzyl-2-[6-(2-chloroacetylamino)-benzothiazol-2-ylsulfanyl]-acetamide | [Molecular Formula]
C18H16ClN3O2S2 | [MDL Number]
MFCD17926346 | [MOL File]
1255099-06-9.mol | [Molecular Weight]
405.92 |
| Hazard Information | Back Directory | [Description]
SKLB-163 is an anticancer agent. It acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK. | [Uses]
SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis[1][2]. | [in vivo]
SKLB-163 (25-100 mg/kg, i.g., once daily for 30 days) inhibits tumor growth and ascites formation, and inhibits liver and lung metastasis in NPC lung metastatic mice model[1].
SKLB-163 (50 mg/kg, once daily. from the 6th day of SKLB-163 administration, 3 Gy radiation once per day for 3 days) sensitizes NPC tumor to irradiation in CNE-2 and C666-1 subcutaneous xenograft mice models[1].
| Animal Model: | NPC lung metastatic model: transplanting NPC cells C666-1 into the livers of BALB/c nude mice[1] | | Dosage: | 25, 50, 100 mg/kg | | Administration: | intragastric administration, once daily for 30 days | | Result: | Reduced tumor size by 33.5% (25 mg/kg), 53.6% (50 mg/kg), 81.6% (100 mg/kg), respectively.
Ascited formation by 33.9% (25 mg/kg), 58.7% (50 mg/kg), 82.2% (100 mg/kg).
Inhibited liver or lung metastasis. |
| [References]
[1] He J, et al. Antitumor and radiosensitizing effects of SKLB-163, a novel benzothiazole-2-thiol derivative, on nasopharyngeal carcinoma by affecting the RhoGDI/JNK-1 signaling pathway. Radiother Oncol. 2018 Oct;129(1):30-37. DOI:10.1016/j.radonc.2018.02.007
[2] Peng X,et al. SKLB-163, a new benzothiazole-2-thiol derivative, exhibits potent anticancer activity by affecting RhoGDI/JNK-1 signaling pathway. Cell Death Dis. 2014 Mar 27;5(3):e1143. DOI:10.1038/cddis.2014.107 |
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